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      Multitarget opioid ligands in pain relief: New players in an old game.

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          Abstract

          Still nowadays pain is one of the most common disabling conditions and yet it remains too often unsolved. Analgesic opioid drugs, and mainly MOR agonists such as morphine, are broadly employed for pain management. MOR activation, however, has been seen to cause not only analgesia but also undesired side effects. A potential pain treatment option is represented by the simultaneous targeting of different opioid receptors. In fact, ligands possessing multitarget capabilities led to an improved pharmacological fingerprint. This review focuses on the examination of multitarget opioid ligands which have been distinguished in peptide and non-peptide and further listed as bivalent and bifunctional ligands. Moreover, the potential of these compounds, both as analgesic drugs and pharmacological tools to explore heteromer receptors, has been stressed.

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          Author and article information

          Journal
          Eur J Med Chem
          European journal of medicinal chemistry
          Elsevier BV
          1768-3254
          0223-5234
          Jan 27 2016
          : 108
          Affiliations
          [1 ] Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy. Electronic address: rita.turnaturi@tiscali.it.
          [2 ] Department of Drug Sciences-Medicinal Chemistry Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
          [3 ] Department of Drug Sciences-Pharmacology and Toxicology Section, University of Catania, Viale A. Doria 6, 95125 Catania, Italy.
          Article
          S0223-5234(15)30365-2
          10.1016/j.ejmech.2015.11.028
          26656913

          KOR, DOR, Bivalent ligands, Bifunctional ligands, Pain, MOR

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